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| Clinical data | |
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| Trade names | Rudotel |
| AHFS/Drugs.com | International Drug Names |
| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Bioavailability | 50–75% (Сmax = 1–2 hours) |
| Protein binding | >99% |
| Metabolism | Hepatic |
| Eliminationhalf-life | 2 hours, 36–150 hours (terminal) |
| Excretion | Renal (63–85%),Biliary 15–37% |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.018.895 |
| Chemical and physical data | |
| Formula | C16H15ClN2 |
| Molar mass | 270.76 g·mol−1 |
| 3D model (JSmol) | |
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Medazepam is a drug that is abenzodiazepine derivative. It possessesanxiolytic,anticonvulsant,sedative, andskeletal muscle relaxant properties. It is known by the following brand names:Azepamid,Nobrium,Tranquirax (mixed withbevonium),Rudotel,Raporan,Ansilan andMezapam.[2] Medazepam is a long-acting benzodiazepine drug. The half-life of medazepam is 36–200 hours.[3]
Medazepam acts as aprodrug tonordazepam.Benzodiazepine drugs including medazepam increase the inhibitory processes in the cerebral cortex by allosteric modulation of the GABA receptor.[4] Benzodiazepines may also act viamicromolar benzodiazepine-binding sites asCa2+ channel blockers and significantly inhibited depolarization-sensitive calcium uptake in experiments with cell components from rat brains. This has been conjectured as a mechanism for high dose effects against seizures in a study.[5] It has major active benzodiazepine metabolites, which gives it a more prolonged therapeutic effect after administration.[6]